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| Targets |
OX04528 targets G protein-coupled receptor 84 (GPR84), a member of the class A GPCR family that is activated by medium-chain fatty acids. GPR84 is involved in various physiological processes, including immune responses, inflammation, and metabolism. OX04528 acts as a biased agonist, preferentially activating G-protein signaling pathways over β-arrestin recruitment. By binding to GPR84, OX04528 inhibits forskolin-induced cAMP production in cells expressing the receptor. The compound's potent inhibition of cAMP production with an EC50 of 5.98 pM demonstrates its high efficacy at the receptor. The compound also exhibits off-target inhibition of the renal outer medullary potassium channel ROMK1 (Kir1.1).
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| ln Vitro |
In vitro, OX04528 demonstrates potent agonist activity at GPR84 with an EC50 of 5.98 pM for inhibition of forskolin-induced cAMP production in CHO-hGPR84 cells. The compound is highly selective for GPR84, showing no activity at GPR40, GPR120, or CB2 receptors. It exhibits no detectable effects on β-arrestin recruitment, confirming its G-protein-biased signaling profile. OX04528 has no cytotoxicity. The compound's off-target inhibition of the renal outer medullary potassium channel ROMK1 (Kir1.1) with nanomolar potency distinguishes it from other in-class GPR84 agonists. These in vitro activities make OX04528 a valuable tool for studying GPR84 biology and its role in cancer and other diseases.
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| ln Vivo |
In vivo, OX04528 is an orally active compound. As a potent GPR84 agonist, it would be expected to modulate GPR84-mediated signaling pathways in vivo, potentially affecting immune responses, inflammation, and cancer-related processes. However, specific animal model studies, dosing regimens, and quantitative outcomes have not been extensively reported in the available literature. The compound's oral bioavailability and G-protein-biased signaling profile suggest that it may have favorable pharmacokinetic and pharmacodynamic properties for in vivo studies. Further in vivo studies would be required to fully characterize its efficacy, safety, and pharmacokinetic properties in various disease models. The compound is intended for research use only.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for OX04528 typically involve measuring its agonist activity at GPR84 using cell-based functional assays. A standard protocol would involve using CHO cells stably expressing human GPR84. Cells are seeded in multi-well plates and treated with varying concentrations of OX04528 (typically 0.001 nM to 10 μM) in the presence of forskolin (e.g., 25 μM) to stimulate cAMP production. The amount of cAMP produced is measured using a competitive ELISA or a homogeneous time-resolved fluorescence (HTRF) assay. The inhibition of forskolin-induced cAMP production by OX04528 is calculated, and EC50 values are determined from concentration-response curves. For selectivity profiling, similar assays are performed using cells expressing other GPCRs such as GPR40, GPR120, and CB2. β-arrestin recruitment can be assessed using PathHunter or similar assays.
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| Cell Assay |
In vitro cell-based assay protocols for OX04528 typically involve assessing its effects on GPR84-mediated signaling in cultured cells. A standard protocol would involve seeding CHO cells stably expressing human GPR84 in 96-well plates. Cells are treated with varying concentrations of OX04528 (typically 0.001 nM to 10 μM) for a defined period (e.g., 30 minutes), and intracellular cAMP levels are measured using a competitive immunoassay or HTRF assay. The inhibition of forskolin-induced cAMP production is calculated. For cell viability studies, cells are treated with OX04528, and viability is assessed using MTT or CellTiter-Glo assays. For selectivity studies, the compound's activity is assessed in cells expressing other GPCRs. Appropriate controls include vehicle-treated cells and cells treated with a known GPR84 agonist.
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| Animal Protocol |
In vivo animal experimental protocols for OX04528 have not been extensively reported in the available literature. As an orally active GPR84 agonist, potential studies might involve administering the compound to animal models of cancer, inflammation, or metabolic diseases. A hypothetical protocol for studying its anti-tumor effects would involve implanting tumor cells (e.g., xenograft models) in immunodeficient mice, allowing tumors to reach a certain size, and then administering OX04528 via oral gavage at doses determined from preliminary pharmacokinetic and tolerability studies. Treatment would typically be administered daily for 2-4 weeks. Endpoints would include tumor volume measurement, tumor weight at necropsy, assessment of GPR84 signaling in tumor tissues, and evaluation of immune cell infiltration. For inflammation studies, the compound could be administered in models of inflammatory disease. However, specific published protocols are not available.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OX04528 indicate that the compound is orally active and bioavailable. It has a molecular weight of 365.27 and a molecular formula of C16H13F6NO2. The compound is typically stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. Specific PK parameters such as half-life, Cmax, AUC, volume of distribution, and clearance have not been extensively reported. The compound's metabolism, protein binding, and routes of elimination remain to be characterized. Further pharmacokinetic studies would be required to understand its absorption, distribution, metabolism, and excretion profile. The compound is intended for research use only and is not intended for human use.
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| Toxicity/Toxicokinetics |
Toxicological data for OX04528 are limited, as the compound is intended for research use only and has not undergone systematic toxicity testing. No acute toxicity (LD50), subchronic toxicity, genotoxicity, or reproductive toxicity studies have been reported specifically for this compound. The compound has no cytotoxicity, suggesting a favorable safety profile in vitro. However, the compound's off-target inhibition of the renal outer medullary potassium channel ROMK1 (Kir1.1) with nanomolar potency may have implications for renal function and requires further investigation. The compound is not intended for human use. Researchers should follow standard safety precautions when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact.
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| References | |
| Additional Infomation |
OX04528 is a research-grade compound that functions as a potent, G-protein-biased, and orally active GPR84 agonist. It inhibits cAMP production with an EC50 of 5.98 pM and is highly selective for GPR84 over GPR40, GPR120, and CB2. The compound has no detectable effects on β-arrestin recruitment and exhibits off-target inhibition of ROMK1 (Kir1.1). OX04528 may be useful in cancer research. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves biased agonism at GPR84, preferentially activating G-protein signaling pathways. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
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| Molecular Formula |
C16H13F6NO2
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| Molecular Weight |
365.27
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| CAS # |
3028055-45-7
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~273.77 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7377 mL | 13.6885 mL | 27.3770 mL | |
| 5 mM | 0.5475 mL | 2.7377 mL | 5.4754 mL | |
| 10 mM | 0.2738 mL | 1.3689 mL | 2.7377 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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